Overview of P-glycoprotein inhibitors: a rational outlook

  • Kale Mohana Raghava Srivalli Osmania University; G. Pulla Reddy College of Pharmacy; Department of Pharmaceutics
  • P. K. Lakshmi Osmania University; G. Pulla Reddy College of Pharmacy; Department of Pharmaceutics
Keywords: P-glycoprotein^i1^sinhibit, Multidrug resistence, Cluster of differentiation 243, Sphingolipids, Competitive inhibitors


P-glycoprotein (P-gp), a transmembrane permeability glycoprotein, is a member of ATP binding cassette (ABC) super family that functions specifically as a carrier mediated primary active efflux transporter. It is widely distributed throughout the body and has a diverse range of substrates. Several vital therapeutic agents are substrates to P-gp and their bioavailability is lowered or a resistance is induced because of the protein efflux. Hence P-gp inhibitors were explored for overcoming multidrug resistance and poor bioavailability problems of the therapeutic P-gp substrates. The sensitivity of drug moieties to P-gp and vice versa can be established by various experimental models in silico, in vitro and in vivo. Ever since the discovery of P-gp, the research plethora identified several chemical structures as P-gp inhibitors. The aim of this review was to emphasize on the discovery and development of newer, inert, non-toxic, and more efficient, specifically targeting P-gp inhibitors, like those among the natural herb extracts, pharmaceutical excipients and formulations, and other rational drug moieties. The applications of cellular and molecular biology knowledge, in silico designed structural databases, molecular modeling studies and quantitative structure-activity relationship (QSAR) analyses in the development of novel rational P-gp inhibitors have also been mentioned.


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How to Cite
Srivalli, K., & Lakshmi, P. (2012). Overview of P-glycoprotein inhibitors: a rational outlook. Brazilian Journal of Pharmaceutical Sciences, 48(3), 353-367. https://doi.org/10.1590/S1984-82502012000300002